Inhibition of growth of Toxoplasma gondii by qinghaosu and derivatives.
The antimalarial compound qinghaosu (artemisinin) was tested in vitro for the ability to inhibit plaque formation by Toxoplasma gondii in fibroblasts. Qinghaosu at 0.4 microgram/ml for 5 days eliminated all plaques and microscopic foci of T. gondii. At 1.3 micrograms/ml for 14 days, qinghaosu completely eliminated T. gondii. Pretreatment of host cells or T. gondii with qinghaosu had no effect on T. gondii growth. There was no apparent toxicity to human fibroblasts in long-term studies. Of the six qinghaosu derivatives tested, dihydroqinghaosu, 1-propyl-ether-qinghaosu, and 1-butyl-ether-qinghaosu were comparable to qinghaosu. Ethyl-ether-qinghaosu (arteether) and sec-butyl-ether-qinghaosu were more effective. Methyl-ether-qinghaosu (artemether) was the most effective, with a potency approximately 10-fold greater than that of qinghaosu.
Ke
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Department of Infectious Diseases, First Affiliated Hospital, Hunan Medical University, People's Republic of China.
Krug
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EC
Marr
J J
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Berens
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D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D037621:Artemisinins; D002478:Cells, Cultured; D005347:Fibroblasts / Q000187:drug effects; D006801:Humans; D012717:Sesquiterpenes / Q000494:pharmacology*; D014122:Toxoplasma / Q000187:drug effects* / Q000254:growth & development; D010948:Viral Plaque Assay
D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; C031327:artemisinin